[CAS NO. 942398-84-7]  Amiselimodhydrochloride

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PRODUCTS SPECIFICATIONS [942398-84-7]

Catalog
HY-16734A
Brand
MCE
CAS
942398-84-7

DESCRIPTION [942398-84-7]

Overview

MDLMFCD25372041
Molecular Weight413.90
Molecular FormulaC19H31ClF3NO3
SMILESOCC(CCC1=CC=C(OCCCCCCC)C(C(F)(F)F)=C1)(N)CO.[H]Cl

For research use only. We do not sell to patients.

Summary

Amiselimod hydrochloride is a novel sphingosine 1-phosphate receptor-1 (S1P1) modulator, designed to reduce the bradycardia effects associated with fingolimod and other S1P receptor modulators. target: S1P1 In vivo: After oral administration of amiselimod or fingolimod at 1 mg/kg, the concentration of amiselimod-P in rat heart tissue was relatively lower than that of fingolimod-P, potentially contributing to the minimal cardiac effects of amiselimod. Amiselimod-P showed potent selectivity for S1P1 , high selectivity for S1P5 , minimal agonist activity for S1P4 , no distinct agonist activity for S1P2 or S1P3 , and approximately 5-fold weaker GIRK activation than fingolimod-P. [1] Amiselimod 0·2 mg and 0·4 mg significantly reduced the total number of gadolinium-enhanced T1-weighted lesions. [2]


Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT02389790 Mitsubishi Tanabe Pharma Corporation
Crohn´s Disease
August 2015 Phase 2
NCT01666327 Mitsubishi Tanabe Pharma Corporation
Inflammatory Bowel Disease
June 2012 Phase 1
NCT02148185 Mitsubishi Tanabe Pharma Corporation
Crohn´s Disease
May 2014 Phase 1

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)


Solvent & Solubility

In Vitro:

DMSO : 110 mg/mL ( 265.76 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4160 mL 12.0802 mL 24.1604 mL
5 mM 0.4832 mL 2.4160 mL 4.8321 mL
10 mM 0.2416 mL 1.2080 mL 2.4160 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.75 mg/mL (6.64 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.75 mg/mL (6.64 mM); Clear solution

* All of the co-solvents are available by MCE.